Investigations designed to address the completion of the total synthesis of the antitumor antibiotic CC-1065, the continuation and completion of structure-activity studies on CC-1065, and the initiation of efforts of the design, synthesis and evaluation of synthetic topological agents structurally related to CC-1065 as potential high-affinity, sequence-selectively, B-DNA binding agents are detailed. The initiation of efforts on the total sythesis of bleomycins (glycopeptide antitumor-antibiotics), and the initiation of structure activity studies employing synthetic bleomyins, are detailed.